WO2011059416A1

WO2011059416A1 - Prophylactic antioxidant agent for protecting the tissues of an organism from the action of negative ecological factors or the consequences of smoking tobacco

Info

Publication number: WO2011059416A1
Application number: PCT/UA2010/000051
Authority: WO
Inventors: Владыслав РОЗЕНФЕЛЬД; Сэргий ДЯЧЕНКО
Original assignee: Rozenfeld Vladislav; Dyachenko Sergiy
Priority date: 2009-11-11
Filing date: 2010-08-09
Publication date: 2011-05-19
Also published as: TR201205418T1; RU2012109253A; UA95139C2

Abstract

The invention relates to pharmacology, medicine, livestock breeding and poultry farming, and is directed towards producing agents and methods which can be used for prophylactic aims in order to reduce the risk of morbidity caused by negative ecology and by active or passive smokers breathing in tobacco smoke. The claimed prophylactic antioxidant agent contains sodium 2, 3-dimercaptopropane sulphonate and a pharmaceutically acceptable carrier. The agent effectively protects the tissues of an organism from the action of negative ecological factors or the consequences of smoking tobacco. Furthermore, the claimed agent can be used effectively in livestock breeding and poultry farming in order to increase productivity and reduce the death rate of animals and birds.

Description

Antioxidant prophylactic to protect body tissues from the effects of negative environmental factors or the effects of smoking

FIELD OF TECHNOLOGY

The invention relates to pharmacology, medicine, animal husbandry, poultry, and is aimed at creating tools and methods that can be used prophylactically to reduce the risk of morbidity caused by negative ecology, as well as inhalation, by active or passive smokers, of tobacco smoke.

BACKGROUND OF THE INVENTION

It is known that tobacco smoke contains a large number of carcinogens, among which there are compounds of mercury, chromium, nickel, lead, and iron. Heavy metals, depending on the concentration in the human body, can directly or indirectly damage DNA, that is, all heavy metals are genotoxic, as well as all of them are immunotoxic and are also carcinogens. Scientists have established the fact that the more heavy metals in the human body, the more the activity of free radicals. Getting into the human body with tobacco smoke, free radicals can cause many dangerous diseases (such as cancer), because their action is unlimited, and all cells of the body suffer. The harmful effect of free radicals is manifested in accelerating the aging of the human body, in provoking inflammatory processes in different organs and tissues, in disrupting the functioning of different organ systems. Tobacco smoke can cause damage to the gums, it leads to diseases such as bleeding gums, gingivitis, periodontitis by reducing the level of antioxidant capabilities of the body. Smoking combined with low levels of antioxidants increases the likelihood of prostate cancer. The effects of smoking and the low status of antioxidants on the bronchopulmonary system are also unfavorable. The pharmacological effects of heavy and radioactive metals reduce the activity of natural antioxidants, in particular those that contain SH groups, toxic metabolites quickly deplete their supply, and oxidative stress is developing.

In addition, city dwellers inhale heavy metals during outdoor walks. Heavy metals are the most dangerous component of exhaust gases. Small particles of inorganic and organic metal compounds are suspended in the air we breathe. Lead negatively affects the functioning of the central nervous system. If it enters the human body, it can lead to headaches, fatigue, hearing loss, memory, and colloquial speech. In addition, lead also negatively affects many other human organ systems.

At the moment, paper filters are used to reduce heavy metals getting into the tissues of the smoker’s body, which bind heavy metals by mechanical filtration and only partially cope with their task.

The applicant is not aware of preventive measures to protect internal organs from the effects of negative environmental factors or the effects of smoking.

SUMMARY OF THE INVENTION

The basis of the invention is the task of creating a prophylactic agent that will reduce the likelihood of diseases that arise as a result of heavy metals entering the body tissue from the circulatory system, in particular mercury, chromium, nickel, lead, iron and their compounds.

The problem is solved by a prophylactic antioxidant to protect body tissues from the effects of negative environmental factors or the effects of smoking so that it contains 2,3-dimercaptopropanesulfonate sodium and a pharmaceutically acceptable carrier.

As a pharmaceutically acceptable carrier, the agent may contain excipients selected from the group consisting of a binding agent and / or a filler and / or lubricant and / or disintegrant and / or wetting agent and / or inert solvent and / or a surface active agent and / or a dispersing agent and / or a suspending agent and / or an emulsifying agent and / or an edible oil and / or a flavoring substance and / or food coloring.

The use of the claimed prophylactic agent provides a multiple reduction in the ingress of mercury, chromium, nickel, lead and iron, as well as their compounds, into the tissues of the body, including active and passive smokers, and the associated reduction in the risk of diseases and increased antioxidant protection of the body. Sodium 2,3-dimercaptopropanesulfonate (unitiol) has the structural formula:

H - CH - CH - CH ₂ - S0 ₃ Na

· | - |

SH SH

According to the mechanism of action, this is a complexon that has an antioxidant effect (see patent of the Russian Federation Ν ”2195255, as well as: Zenovich SM and others. Study of antioxidant properties of unitiol in experimental post-drug detoxification. Journal“ Narcology ”N2 4, 2004, p. . 30-33). Its active sulfhydride groups react with thiol poisons, which are found in the blood or tissues and form non-toxic complexes with them, which are excreted in the urine. The use of unitiol as an antidote is known for heavy metal poisoning (see MD Mashkovsky. Register of Medicines of Russia. Publishing House "Encyclopedia of Medicines", M., ed. 7th, 2000, p. 949). Unithiol is used to treat acute and chronic poisoning with compounds of arsenic, mercury, chromium, bismuth and other metals, which belong to the so-called thiol poisons, that is, substances that are able to interact with sulfhydride (thiol) groups of enzyme proteins and inactivate them.

All the described actions occur after poisoning the body with heavy metals. It is known that when heavy metals get into the body’s tissues, they cause tissue destruction, and if this destructive effect is not stopped, this leads to severe intoxication of the body and, as a possible consequence, to a fatal result. In these cases, different antidotes are used, in particular, unitiol. But toxic substances, including heavy metals, in the above cases, are excreted after they have already entered the tissues of the body and caused damage there. After applying the antidote, the tissues remain affected, which, of course, affects human health.

Unlike the known one, the claimed solution proposes a prophylactic agent that contains unitiol and a pharmaceutically acceptable carrier, and this agent is intended for use in small doses until the body is poisoned with the above metals and their compounds, that is, before tissue damage.

Pharmacodynamics: the active unitiol sulfhydride groups, taken in the morning by a smoker or resident of an ecologically unfavorable region, enter the bloodstream, where they “expect” heavy and radioactive metals to be released in connection with a smoked cigarette or the atmosphere they inhale. Having met in the blood, they form non-toxic compounds (complexes), which are excreted urine. Thus, the goal has been achieved - a significant part of the heavy metals, trapped in the blood, has no chance of getting into the tissues of the body. However, unitiol interacts not only with free arsenic compounds and heavy metal ions that are in the blood and tissues, but also with those that have already entered into interaction with enzymes and other protein substances in the body. In this case, sulfhydride groups of proteins previously associated with metal ions are released, and their function is resumed.

In addition, unithiol, as an antioxidant, minimizes the negative effects on the smoker's body of free radicals, which are found in large quantities in tobacco smoke

It is also believed that with frequent or very prolonged use, unitiol can remove cations of copper, manganese and zinc from the body. However, the company HEYL, which produces DIMAVAL (a synonym for unitiol), claims that its experiments on the introduction of 15 mg per kg of body weight for six months did not reveal any histological or biochemical abnormalities. Given these discrepancies, it is necessary to periodically, every 3 months, check the mineral balance of the body, and in case of a deficiency, it is necessary to make up for it by adopting an appropriate complex of trace elements.

A patent for utility model of Ukraine N ° 4491 is known, which describes a method of reducing the negative effect of T-2 toxin on an animal organism by introducing unitiol to an animal that is chronically poisoned. T-2 toxin belongs to the toxic mycotoxins of the trichocetene group, which are formed as a result of the activity of molds of the genus Fusarium.

Mycotoxins are toxic compounds of fungal mold. The danger of mycotoxins is due to the fact that when processing food or feed some of them do not break up. Such compounds have a harmful effect on the liver, kidneys, spleen of people and animals, weaken the immune system, cause cancer, affect the ability to reproduce. Mycotoxins can be found in nuts, grains, cocoa and coffee grains, oilseeds, some vegetables and fruits, as well as in animal products - meat, fat, blood.

A patent is known for utility model of Ukraine Ns 10344, which describes a method for treating livestock with acute nitrate toxicosis using unitiol.

In agriculture, chemicals are widely used - mineral fertilizers and preparations for the destruction of weeds, crop pests and animal parasites. The use of these substances in combination with other measures can increase the yield and productivity of animals. But in the vast majority of cases, chemicals and fertilizers are poisonous and potent substances. So, sodium arsenite and Parisian herbs contain arsenic; granozan and morcuran - mercury.

MODES FOR CARRYING OUT THE INVENTION

Example 1

Prepared a prophylactic for the protection of internal organs in the form of pills with the following components in each pill, mg:

2,3-dimercaptopropanesulfonate sodium

(in terms of anhydrous substance) 20 milk sugar 65 corn starch 13

magnesium stearate 1 aerosil 1 Example 2

2,3-dimercaptopropanesulfonate sodium

(in terms of anhydrous substance) 75 milk sugar 75 corn starch 13

magnesium stearate 1 aerosil 1

Example 3

Prepared a prophylactic for the protection of internal organs in the form of pills with the following components in each pill, mg: 2,3-dimercaptopropanesulfonate sodium

(in terms of anhydrous substance) 60 milk sugar 85 corn starch 13

magnesium stearate 1 aerosil 1

Example 4

Prepared a prophylactic for the protection of internal organs in the form of capsules with the following components, mg:

Sodium 2,3-dimercaptopropanesulfonate 10 gelatin capsule ^ 63

Example 5

2,3-dimercaptopropanesulfonate sodium 100 gelatin capsule. 97 Example 6

Sodium 2,3-dimercaptopropanesulfonate 50 gelatin capsule 75

Example 7

Prepared a prophylactic to protect internal organs in the form of an aqueous solution with the following components:

2,3-dimercaptopropanesulfonate sodium 5% water 95%

Examples that confirm the effectiveness of the claimed prophylactic agent:

Example 8

The patient, 45 years old, male, actively smokes 25 years. Urinalysis after the patient smokes 20 cigarettes per day, has the following indicators, mg / l:

Hg - 0, 0002; Cr <0.001; Ni is 0.16; Pb - 0.002; Fe - 0.084.

The patient began to take daily one morning a pill with a unitiol content of 60 mg (Example 3). Once a week, the patient carried out daily urine collection for analysis on the content of heavy metals. Weighted average test results, mg / l: Hg - 0, 0009; Cr - 0.003; Ni - 0.426; Pb - 0.005; Fe - 0.226.

Urine analysis indicators indicate that due to the use of the claimed drug, the amount of mercury that is excreted from the body increased by 350% relative to control, by 200% by chromium, by 150% by nickel, lead and iron. After ingestion of one capsule, which contains 60 mg of unitiol, its maximum concentration in the blood is reached after 1.5 hours. and is within 30 mg / l. Average time stay of the drug in the body for 9-12 hours. During this time, the patient smokes cigarettes, which leads to the ingress of heavy metals through the lungs, first into the smoker's blood, and then partially into the tissues of his body. In our case, the active unithiol sulfhydride groups, interacting with the venom poisons that are in the blood, form non-toxic compounds (complexes) with them, which are excreted in the urine, which is confirmed by laboratory studies.

Example 9

The patient, 35 years old, a woman, actively smokes 10 years. Urinalysis after the patient smokes 10 cigarettes per day, has the following indicators, mg / l: Hg - 0, 0001; Cr <0.001; Ni is 0.15; Pb - 0.003; Fe - 0.06.

The patient began to take 3 gelatin capsules daily with a total content of unitiol 30 mg daily in the morning (example 4). Once a week, the patient carried out daily urine collection for analysis on the content of heavy metals.

Weighted average test results, mg / l: Hg - 0, 0006; Cr - 0.004; Ni - 0.315; Pb - 0.006; Fe - 0.18.

Analysis of her urine testifies to the fact that thanks to taking the declared prophylactic, the amount of mercury that is excreted from the body increased by 500% relative to control, chromium by 300%, nickel by 100%, lead by 100%, and iron - by 200%.

Example 10

Experimental studies of the qualities of the declared prophylactic agent were also carried out on broiler birds at the Stavropol Broiler factory. The experiments were carried out in three poultry houses with 18,000 birds each. In each of the poultry houses, 2 lots were allocated: control and experimental, 9000 goals in each. Experienced batch of broilers gave an aqueous solution of the claimed funds at the rate of approximately 1.5 mg per 1 kg of live weight of the bird daily.

There were packaged unitiol consumption packages based on poultry growth for each house. The amount of unitiol in grams is presented in table 2.

In the morning the poultry house poured Unitiol from a prepared bag into a liter vessel with water. This solution was added to the water supply system. The chicks drank a prophylactic with a drink. The results are shown in table 1.

The studies showed the following results.

House JVa 1.

Case 28. Drinking within 14 days.

In accordance with table 2, unitiol costs per 9000 goals, the costs amounted to 38.3 g unitiol or 919 rubles, when the price for unitiol is 24,000 Russian rubles per kg. According to the data given in table 1, the increase in the amount of meat, which is calculated on the basis of the gain and the reduction in mortality, is 9,000 heads respectively: 1.2% of meat or 214 kg, or 14,689 rubles, in wholesale prices (gain of 20 g - 1 % and survival rate of 0.2%, in the amount of 1, 2%, based on the selling price of 88 rubles per kg and meat yield of 78%). Net profit, which is obtained by subtracting the cost of unitiol from the added value of meat, and profitability, by corps, based on 9000 goals: 13770 rubles or 1498% profitability.

House JVg 2.

Case 31. Drinking within 21 days.

In accordance with the table of unitiol costs based on 9000 goals, the costs amounted, at a unitiol price of 24,000 Russian rubles per kg, respectively, 100 g of unitiol or 2400 rubles. According to the data given in table 1, the increase in the amount of meat that comes out of the calculation of the gain and the reduction in mortality, respectively, for 9000 heads: 1.9% meat or 388 kg, or 26644 rubles in wholesale prices (weight gain of 25 g - 1.1% and survival rate of 0.8%, in the amount of 1, 9%, based on the selling price of 88 rubles for kg and meat yield 78%). Net profit, which is obtained by subtracting the cost of unitiol from the added value of meat, and profitability, by buildings, based on 9000 heads: 24,244 rubles or 1010% profitability.

House JVg 3.

Case 5. Drinking within 35 days.

In accordance with the table of unitiol costs based on 9000 goals, the costs amounted, at a unitiol price of 24,000 Russian rubles per kg, respectively, 374 g unitiol or 8976 rubles. According to the data given in table 1, the increase in meat, which is calculated on the basis of the gain and decrease in mortality, is, respectively, by 9000 heads: 1.9% of meat or 349 kg, or 23955 rubles, in wholesale prices (gain 40 g - 1 , 9% and survival rate of 0.8%, in the amount of 1.9%, based on the selling price of 88 rubles for kg and meat yield 78%). Net profit, which is obtained by subtracting the cost of unitiol from the added value of meat, and the profitability of the buildings, based on 9000 heads: 14,979 rubles, or 167% of profitability.

After the experiments, we analyzed the contents of mercury, cadmium, and lead in the tissues of bird organisms of the experimental and control groups. The results are shown in table 3. The data shown in table 3 show that broiler meat that took unitiol contains less than 45% mercury, 50% less cadmium, and 25% less lead.

Example 11

There have been studies of the claimed funds in adult hens at the Staritsa poultry farm (Ukraine). The experiment was conducted on 9 houses, of which house N <> 1 was experimental, the other 8 - control The birds of the parent herd were given the claimed amount in the same quantities as the broilers at the Stavropol Broiler factory and in the same way. The data are shown in tables 4-7.

Studies have shown the following:

1. According to the first poultry house, before applying the claimed remedy, mortality exceeded twice the weighted average, and after its application, mortality decreased to the weighted average.

2. Before the application of the claimed product, according to the first house, the average weight of the chicken was below the weighted average by 5%, and after application - only 2%.

3. The average rate of weight gain during the period of taking the drug in the control groups was 29%, while the average rate of weight gain during the period of taking the drug in the experimental group was 32.6%. From this we can conclude that the positive derivative of the rate of mass growth (relative to control) was 12.4%.

4. Improved feed conversion rates. This is obvious from such calculations: the average consumption of control chicken over a 70-day period was (129 g +161 g) / 2 x 70 days = 10150 g of feed. The average consumption of chicken from the experimental group over a 70-day period was (129 g +166 g) 12 x 70 days = 10325 g of feed. Based on the growth statistics for the control (850 g = 3780 g - 2930 g) and experimental (910 g = 3700 g - 2790 g) groups, we can calculate that the feed conversion for control is 11.94 (dividing 10150 g of feed by 850 g growth), and for the experimental group - 1.35 (dividing 10325 g of feed by 910 g of growth), from which we can conclude that the conversion of feed is reduced by 5.2%), which reduces the cost of keeping chickens.

5. In terms of egg production, the worst house showed results that exceed the weighted average of other houses by 4.75%. In fact, only this parameter gives one chick from a chicken. additionally a month, which pays off twice the use of the tool that is claimed.

Based on the studies, we can conclude that the use of the claimed funds:

- increases egg production by more than 4.75%;

- reduces feed conversion by 5.2%;

- gives a positive derivative of the rate of mass growth (relative to control) 12.4%;

- reduces herd mortality.

INDUSTRIAL APPLICABILITY

The preparations can be made in the form of tablets, capsules, injection solutions or can be given in the form of an aqueous solution to a bird or animal.

Experiments with the use of the drug "unitiol"

Table 1

Table 1 (continued)

Unitiol consumption per 9000 birds

table 2

Continuation of table 2

Continuation of table 2

room

32 33 34 35 Total:

the package

Consumption

unitiola, 23.616 24.813 26.028 27.234 374.076

g The content of heavy metals in the biomaterial of the liver of broiler chickens

Table 3

Percentage of performance for 24 and 34 weeks

Table 4

Live weight of the bird for 24 and 34 weeks

Table 5

Continuation of table 5

Poultry departure from week 20 to week 24

Table 6

Poultry departure from week 25 to 34

using unitiol on the 1st house

Table 7

Claims

Claim

A prophylactic is an antioxidant to protect body tissues from the effects of negative environmental factors or the effects of smoking, characterized in that it contains 2,3-dimercaptopropanesulfonate sodium and a pharmaceutically acceptable carrier.